Table 1.
PI3K/AKT/mTOR pathway inhibitors.
| Inhibitors | Targets | FDA-approved status | Clinical trial | Condition |
|---|---|---|---|---|
| Piqray (alpelisib) 2019 year |
PI3Kα | Yes | NCT02437318(Phase III) | In combination with fulvestrant for postmenopausal women, and men, with HR-positive, HER2-negative, PIK3CA-mutated, advanced or metastatic breast cancer. |
| Copiktra (duvelisib) 2018 year |
PI3Kδ, PI3Kγ | Yes | NCT02004522(Phase III);NCT02204982(Phase III) | Adult patients with relapsed or refractory CLL or SLL or FL after at least two prior therapies. |
| Aliqopa (copanlisib) 2017 year |
PI3Kδ, PI3Kα | Yes | NCT01660451(Phase II) | Copanlisib for the treatment of adult patients with relapsed FL. |
| Zydelig (idelalisib) 2014 year |
PI3Kδ | Yes | NCT01539512(Phase III) | Chronic lymphocytic leukemia, relapsed follicular B-cell non-Hodgkin lymphoma, and relapsed small lymphocytic lymphoma. |
| Ukoniq (umbralisib) 2021year |
PI3Kδ, CK1ε | Yes | NCT02793583 (Phase II/III) | MZL and FL. |
| Sonolisib (PX-866) 2015 year |
PI3Kα, PI3Kγ, PI3Kδ | No | NCT01259869(Phase II) | Glioblastoma multiforme at the time of first relapse or progression. |
| Buparlisib (NVP-BKM120) 2018 year |
PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ | No | NCT01633060(Phase III) | In combination fulvestrant, in postmenopausal women with HR-positive HER2-negative aromatase inhibitor-treated, locally advanced or metastatic breast cancer who progressed on or after mTOR inhibitor-based treatment. |
| Afinitor (everolimus) 2009 year |
mTORC1, mTORC2 | Yes | NCT00863655(Phase III); NCT00510068(Phase III); NCT01524783(Phase III); NCT00412061(Phase III); NCT00410124(Phase III) | Advanced HR+, HER2- breast cancer; PNET; progressive NET of gastrointestinal or lung origin; advanced renal cell carcinoma; SEGA and renal angiomyolipomas associated with tuberous sclerosis. |
| Rapamune (Sirolimus) 1999 year |
mTORC1, mTORC2 | Yes | NCT00414648(Phase III) | The prophylaxis of organ rejection in patients aged 13 years or older receiving renal transplants, and LAM. |
| Torisel (temsirolimus) 2007year |
mTORC1, mTORC2 | Yes | NCT00065468(Phase III) | Advanced renal cell carcinoma. |
| Capivasertib (AZD5363) 2020 year |
AKT1, AKT2, AKT3 | No | NCT03997123(Phase III) | Locally advanced or metastatic triple-negative breast cancer |
| Ipatasertib (GDC-0068) 2021 year |
AKT1, AKT2, AKT3 | No | NCT03072238(Phase III) | Ipatasertib plus abiraterone and prednisolone in metastatic castration-resistant prostate cancer |
| MK-2206 2020 year |
AKT1, AKT2, AKT3 | No | NCT01042379(Phase II) | HER2-positive and/or HR-negative breast cancer |
HR: hormone receptor; HER2: epidermal growth factor receptor 2; CLL: chronic lymphocytic leukemia; SLL: small lymphocytic lymphoma; FL: follicular lymphoma; MZL: marginal zone lymphoma; PNET: progressive neuroendocrine tumors of pancreatic origin; NET: neuroendocrine tumors; SEGA: subependymal giant cell astrocytoma; LAM: lymphangioleiomyomatosis.